Synthesis and antibacterial activity of novel modified 5-O-desosamine ketolides

详细信息    查看全文

• 作者：Xiaozhuo Chen^&dagger ; ; Peng Xu^&dagger ; ; Yanpeng Xu ; Lu Liu ; Yi Liu ; Di Zhu ; Pingsheng Lei ; ^{lei@imm.ac.cn}
• 关键词：Desosamine ; Ketolide ; Glycosylation ; Antibacterial activity ; Antibiotic
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 December, 2012
• 年：2012
• 卷：22
• 期：24
• 页码：7402-7405
• 全文大小：284 K

文摘

A series of novel modified 5-O-desosamine-ketolides were synthesized. The 5-O-desosamine fragment was removed from ketolide by an efficient and mild manipulation. 4-O-substituted desosamine was introduced into the ketolide aglycon and various coupling methods were essayed for the glycosylation. Three novel ketolides were tested for in vitro antibacterial activity against a panel of susceptible and resistant pathogens. Compound 26 showed potent activity against all the methicillin-sensitivity and resistant pathogens.